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Publicly Available Published by De Gruyter February 5, 2011

Synthesis of a rhodanine-based compound library targeting Bcl-XL and Mcl-1

Paul H. Bernardo, Thirunavukkarasu Sivaraman, Kah-Fei Wan, Jin Xu, Janarthanan Krishnamoorthy, Chun Meng Song, Liming Tian, Jasmine S. F. Chin, Diane S. W. Lim, Henry Y. K. Mok, Victor C. Yu, Joo Chuan Tong and Christina L. L. Chai

A small library of pyridine-based rhodanine analogues of BH3I-1 were synthesized and screened against B-cell lymphoma-extra large (Bcl-XL) and myeloid cell leukemia sequence 1 (Mcl-1) for the ability to displace 5-carboxyfluorescein-labeled Bak peptide (Flu-Bak). Differences in selectivity toward Bcl-XL and Mcl-1 were observed, and the binding modes of selected compounds were studied further. The results may be useful in designing potent small-molecule inhibitors of Bcl-XL and Mcl-1 as well as selective Mcl-1 inhibitors.


Conference

International Conference on Organic Synthesis (ICOS-18), International Conference on Organic Synthesis, ICOS, Organic Synthesis, 18th, Bergen, Norway, 2010-08-01–2010-08-06


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Online erschienen: 2011-2-5
Erschienen im Druck: 2011-2-5

© 2013 Walter de Gruyter GmbH, Berlin/Boston

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